Methods for reducing tackiness associated with a xanthine compound

ABSTRACT

The invention relates to a composition containing, preferably in a physiologically acceptable medium, at least one xanthine base or a plant extract containing it, at least one polyurethane powder, and at least one non-ionic dimethicone copolyol. The invention also relates to a cosmetic method for combating cellulite and/or “orange-peel” skin and/or slimming the figure, comprising the application of the composition to the skin. The composition applied to the skin exhibits good cosmetic properties of softness and of non-tackiness.

REFERENCE TO PRIOR APPLICATIONS

This application claims priority to U.S. Ser. No. 11/305,293 filed Dec.19, 2005, provisional application 60/640,239 filed Jan. 3, 2005, and toFrench patent application 04 53051 filed Dec. 17, 2004, the entirety ofwhich is hereby incorporated by reference.

FIELD OF THE INVENTION

The present invention relates to a composition comprising at least onedimethicone copolyol, at least one xanthine base and at least onepolyurethane powder. The invention also relates to a method forcombating cellulite and/or “orange-peel” skin and/or slimming thefigure, comprising the topical application of the composition to theskin.

Additional advantages and other features of the present invention willbe set forth in part in the description that follows and in part willbecome apparent to those having ordinary skill in the art uponexamination of the following or may be learned from the practice of thepresent invention. The advantages of the present invention may berealized and obtained as particularly pointed out in the appendedclaims. As will be realized, the present invention is capable of otherand different embodiments, and its several details are capable ofmodifications in various obvious respects, all without departing fromthe present invention. The description is to be regarded as illustrativein nature, and not as restrictive.

BACKGROUND OF THE INVENTION

Adiposity (or excess fat in the subcutaneous cellular tissue) can havemany causes that are more or less complex.

Some skin cells, called adipocytes, contain variable amounts of fats inthe form of triglycerides, these triglycerides being synthesized in vivoby the adipocytes themselves, according to enzymatic-type reactions(lipogenesis), from the free fatty acids and the glucose (afterdegradation of the latter to glycerol) contained in the body andintroduced therein through certain foods. Now, in parallel, thetriglycerides thus formed, and then stored, in the adipocyte cells canalso redecompose, still under the action of specific enzymes (lipolysis)contained in these same cells, this time releasing, firstly, fatty acidsand, secondly, glycerol and/or monoesters and/or diesters of glycerol.The fatty acids thus released can then either diffuse in the body inorder to be consumed therein or converted in different ways, or can betaken up again (immediately or a little later) by the adipocytes inorder to again generate triglycerides by lipogenesis.

If, for various reasons (overly rich food, inactivity, ageing and thelike), a substantial imbalance becomes established in the body betweenlipogenesis and lipolysis, i.e., more precisely, if the amounts of fatsformed by lipogenesis become appreciably and constantly greater thanthose which are eliminated by lipolysis, an accumulation oftriglycerides then takes place in the adipocytes, which, if it becomesexcessive, may be reflected gradually by the appearance of thick skin,the surface of which is often non-uniform (“orange-peel skin”) and ofmore or less flaccid or gelatinous consistency, finally giving thefigure a general ungraceful appearance which may evolve from a simplelocal excess (lipodysmorphia) and the formation of cellulite, passingthrough a certain level of stoutness and ending at real obesity.

Now, given in particular the deep discomfort, both physical andaesthetic and sometimes psychological, that adiposity and cellulitecause among individuals who are affected by them, in particular amongwomen, they nowadays constitute a condition that is increasingly lesswell tolerated or accepted.

Solutions have therefore been proposed, in the prior art, forintervening on fatty acid metabolism, which is, as has been seen, one ofthe favoured targets in the control of this excess of fats inadipocytes.

This can be modulated:

-   either by blocking glucose transport inside the adipocyte, which    results, as has been seen, in a decrease in fatty acids entering the    adipocyte,-   or by inhibition of lipoprotein lipase,-   or by activation of triglyceride lipase (or hormone-sensitive    lipase), generally by stimulating cyclic AMP, for example by    activation of adenyl cyclase, or by causing accumulation thereof by    inhibition of phosphodiesterase.

Other biological approaches have been explored for acting on themechanism of lipogenesis and/or of lipolysis. It has thus been proposedto use neuropeptide Y (NPY) receptor antagonists, neuropeptide Y being aneuromediator involved in a certain number of physiological processesand the involvement of which in the regulation of lipolysis it has beenpossible to demonstrate (P. Valet, J. Clin. Invest., 1990, 85, 291-295).It is also possible to use α_(z) receptor antagonists or alternativelyβ3-adrenergic receptor agonists.

The cosmetic compositions proposed to date for the purpose of treatingadiposity therefore contain “slimming” compounds which act on one ormore of the mechanisms mentioned above. Among these, mention may moreparticularly be made of xanthine bases (i.e. xanthine derivatives), suchas theophylline, caffeine, theobromine.

However, xanthine bases such as caffeine have the drawback of conferringon the slimming compositions poor cosmetic properties that areexperienced by the user after application of the composition to theskin. The treated skin exhibits a tacky effect, feels taut and lackssoftness: these harmful properties are not satisfactory to the user.

SUMMARY OF THE INVENTION

One object of the present invention is to provide a composition with aslimming action containing a xanthine base and exhibiting good cosmeticproperties after application of the composition to the skin, inparticular good properties of non-tackiness and of softness.

The inventors have discovered that such a composition can be obtained byusing, with a xanthine base, a polyurethane powder and a non-ionicdimethicone copolyol.

The composition applied to the skin does not exhibit any tacky effectand gives the skin a pleasant feeling of softness, without any effect oftautness. In addition, the composition exhibits good slimmingeffectiveness.

DETAILED DESCRIPTION OF THE PREFERRED EMBODIMENTS

A primary subject of the invention is a composition comprising,preferably in a physiologically acceptable medium, at least one xanthinebase and/or at least one plant extract containing a xanthine base, atleast one polyurethane powder and at least one non-ionic dimethiconecopolyol.

Another subject of the invention is a method for combating celluliteand/or “orange-peel” skin and/or slimming the figure, comprising theapplication to the skin of a composition as defined above.

The composition according to the invention is most preferably generallysuitable for topical application to the skin, and therefore preferablycomprises a physiologically acceptable medium, i.e. a medium compatiblewith the skin. It is preferably a cosmetically acceptable medium, i.e. amedium that has a pleasant colour, smell and feel, and that does notgenerate any unacceptable discomfort (stinging, tautness, redness) thatmay put the consumer off using this composition.

The composition according to the invention comprises at least onexanthine base and/or a plant extract containing it.

Among xanthine bases that can be used according to the invention,mention may be made of: caffeine, theophylline, theobromine, acefylline,xanthinol nicotinate, diniprophylline, diprophylline, etamiphylline andits derivatives, etophylline, proxyphylline, pentophylline,propentophylline, pyridophylline and bamiphylline, and their mixtures,without this list being limiting.

Use is in particular preferably made of caffeine, theophylline,theobromine and acefylline, and more particularly caffeine. Thesexanthine bases are known to be inhibitors of phosphodiesterase, which isthe enzyme responsible for the degradation of cAMP. By increasing theintracellular level of cAMP, these xanthine bases promote lipolyticactivity and therefore constitute first-rate slimming active agents.

As examples of plant extracts containing xanthine bases, mention may inparticular be made of extracts of tea, of coffee, of guarana, of matéand of cola, and their mixtures, without this list being limiting.

The one or more xanthine bases may be present in the compositionaccording to the invention in any amount that is effective for thedesired purpose, for example an amount ranging from 0.01% to 10% byweight, relative to the total weight of the composition, preferablyranging from 0.1% to 7% by weight, and preferentially ranging from 0.1%to 3% by weight, in particular ranging from 1% to 3% by weight.

The composition according to the invention also contains at least onepolyurethane powder. In particular, the polyurethane powder ispreferably not film-forming, i.e. it does not form a continuous filmwhen it is deposited on a support such as the skin.

Advantageously, the polyurethane powder is a powder of a copolymer ofhexamethylene diisocyanate and of trimethylol hexyl lactone. Such apolyurethane powder is in particular sold under the names “PlasticPowder D-400” and “Plastic Powder D-800” by the company Toshiki.

Another polyurethane powder that may be used is that sold under the name“Plastic Powder CS-400” by the company Toshiki.

The at least one polyurethane powder may be present in the compositionaccording to the invention in any amount that is effective for thedesired purpose, for example an amount ranging from 0.5% to 10% byweight, relative to the total weight of the composition, and preferablyranging from 0.5% to 6% by weight, and preferentially ranging from 0.5%to 3% by weight.

The composition according to the invention also comprises at least onenon-ionic dimethicone copolyol.

The non-ionic dimethicone copolyol is an oxypropylenated and/oroxyethylenated polydimethylmethylsiloxane which does not contain anyionic groups (such as anionic, cationic or amphoteric groups).

Non-ionic dimethicone copolyols are in particular described in patentU.S. Pat. No. 4,268,499, the contents of which are incorporated intothis application by way of reference.

A particularly preferred form of dimethicone copolyol is that sold underthe name Dow Corning 5225C by the company Dow Corning.

The one or more non-ionic dimethicone copolyol may be present in thecomposition according to the invention in any amount that is effectivefor the desired purpose, for example in an amount ranging from 0.05% to5% by weight, relative to the total weight of the composition,preferably ranging from 0.1% to 3% by weight, and preferentially rangingfrom 0.1% to 2% by weight.

The composition according to the invention may advantageously comprisean aqueous phase.

For example, the composition may comprise water in an amount rangingfrom 30% to 80% by weight, relative to the total weight of thecomposition, preferably ranging from 40% to 70% by weight, andpreferentially ranging from 45% to 65% by weight.

The water may be normal water, a floral water such as cornflower waterand/or a mineral water such as eau de Vittel, eau de Lucas or eau de LaRoche Posay and/or a spring water, for example.

The aqueous phase may comprise at least one monoalcohol having from 2 to6 carbon atoms, such as ethanol or isopropanol, in particular in anamount ranging from 1% to 30% by weight, relative to the total weight ofthe composition, and preferably ranging from 5% to 20% by weight.

The aqueous phase may also comprise salicylic acid or one of itsderivatives such as n-octanoyl acid, in particular present in an amountranging from 0.1% to 5% by weight, relative to the total weight of thecomposition, preferably ranging from 0.1% to 3% by weight andpreferentially ranging from 0.1% to 2% by weight.

While not bound by any particular theory, it is believed that thepreferred presence of at least one monoalcohol and of salicylic acid inthe aqueous phase promote good dissolving of the xanthine base in theaqueous phase and therefore improve the slimming effectiveness of thecomposition.

The composition according to the invention may be in any form, includingany of the, e.g., cosmetic, dermatological and/or pharmaceutical formsnormally used for topical application to the skin, in particular in theform of an oil-in-water or water-in-oil or multiple emulsion, that isoptionally gelled, of a silicone emulsion, of a microemulsion ornanoemulsion, of a liquid, pasty or solid anhydrous product, or of adispersion of oil in an aqueous phase in the presence of spherules, itbeing possible for these spherules to be polymeric nanoparticles such asnanospheres and nanocapsules or, better still, lipid vesicles of ionicand/or non-ionic type. Advantageously, the composition is in the form ofan oil-in-water emulsion.

The composition of the invention may be more or less fluid and may havethe appearance of a white or coloured cream, of an ointment, of a milk,of a lotion, of a serum, of a paste, of a mousse or of a gel. It mayoptionally be applied to the skin in the form of an aerosol. It may alsobe in the form of a solid, and for example in the form of a stick.

The composition of the invention may also contain the adjuvants known inthe cosmetic and dermatological fields such as hydrophilic or lipophilicgelling agents, hydrophilic or lipophilic active agents, moisturizers(such as glycerol, propylene glycol, butylene glycol, pentylene glycol,hexylene glycol, dipropylene glycol or diethylene glycol), preservingagents, antioxidants, solvents, fragrances, fillers, pigments,hydrophilic screening agents, odour absorbers and dyestuffs. The amountsof these various adjuvants are those conventionally used in the fieldsunder consideration and are, for example, from 0.01 to 20% of the totalweight of the composition. Depending on their nature, these adjuvantscan be introduced into the fatty phase, into the aqueous phase, or intolipid vesicles and/or into nanoparticles.

When the composition according to the invention is an emulsion, theproportion of the fatty phase can preferably range from 5 to 50% byweight, and preferably from 5 to 30% by weight relative to the totalweight of the composition.

As fats that can be used in the invention, use may be made for exampleof mineral oils, oils of animal origin, synthetic oils, silicone oilsand fluoro oils. Fatty acids, waxes and gums, and in particular siliconegums, can also be used as fats.

The emulsifiers and co-emulsifiers optionally used in the composition inthe form of an emulsion include those chosen from those known and usedin the field under consideration. These emulsifiers and co-emulsifiersare preferably present, in the composition, in a proportion ranging from0.3 to 20% by weight, and preferably from 0.5 to 5% by weight relativeto the total weight of the composition. As emulsifiers andco-emulsifiers that can be used in the invention, it is particularlyadvantageous to use the fatty acid esters of a polyol such as PEG-100stearate, PEG-50 stearate and PEG-40 stearate; sorbitan tristearate, theoxyethylenated sorbitan stearates available under the trade names Tween®20 or Tween® 60, for example; and mixtures thereof.

As hydrophilic gelling agents, mention may in particular be made ofcarboxyvinyl polymers (carbomer), acrylic copolymers such asacrylate/alkyl acrylate copolymers, polyacrylamides, polysaccharides,natural gums and clays, and as lipophilic gelling agents, mention may bemade of modified clays such as bentones, metal salts of fatty acids, andhydrophobic silica.

As active agents which will add to the action of the slimming activeagents according to the invention, use may in particular be made of:

-   active agents that act on the microcirculation (vasoprotectors or    vasodilators), such as flavonoids, extracts of Gingko biloba,    ruscogenins, esculosides, escin extracted from horsechestnut,    nicotinates, hesperidin methyl chalcone, butcher's broom, essential    oils of lavender or of rosemary;-   firming active agents and/or anti-glycant active agents (which    prevent the binding of sugar to collagen fibres), such as extracts    of Centella asiatica and of St. Paul's wort, which stimulate    collagen synthesis, silicon, amadorine, vitamin C and its    derivatives and retinol and its derivatives;-   and mixtures thereof.

Of course, those skilled in the art know to choose the optionalcompound(s) to be added to the compositions according to the invention,and also the concentration thereof, in such a way that the advantageousproperties intrinsically associated with the compositions in accordancewith the invention are not, or are not substantially, adversely affectedby the addition envisaged.

The composition defined above can be used to prevent or combat celluliteand/or to refine the figure or the contours of the face.

The invention will now be illustrated by means of the followingnonlimiting examples.

EXAMPLES 1 TO 4

3 slimming compositions according to the invention (Examples 2 to 4)containing a non-ionic dimethicone copolyol and a polyurethane powder,and a composition that is not part of the invention (Example 1)containing an anionic dimethicone copolyol and a silica powder, wereprepared.

The composition was applied to the skin and the cosmetic propertiesobtained were observed.

The contents are expressed in grams.

Example Example Example Example COMPOSITION 1* 2 3 4 PHASE I Water qs qsqs qs Acrylic gelling agent (1) 0.5 0.5 0.2 Xanthan gum 0.1 0.08 AMPS(2) 0.1 1 0.6 Glycerol 4 4 5 4 Propylene glycol 3 3 3 3 Caffeine 2.5 2.53 4 Salicylic acid 0.4 0.4 0.5 0.6 PHASE II Dimethicone copolyol (3) 0 23 5 Volatile silicone oils 9 9 7 5 Pecosil PS-100 (4) 1 — — — Siliconegums 0.5 0.5 1 2 Fragrance 0.4 0.4 0.5 0.5 PHASE III 1 Ethanol 12 12 1618 PHASE IV Polyurethane powder (5) 1 0.8 2 Silica 1 Cosmetic propertiesNo soft Soft Very Very effect. and soft soft The skin slippery skin,skin, catches effect, no no and is not tacky tacky taut. tacky. effect.effect. Tacky sensation. *example not part of the invention (1)Carboxyvinyl polymer sold under the name “Carbopol 980” by the companyNoveon. (2) Polyacrylamidopropanesulphonic acid partially neutralizedwith aqueous ammonia and crosslinked, sold under the name “HostacerinAMPS” by the company Clariant. (3) Mixture of dimethiconecopolyol/cyclopentadimethylsiloxane/water (10/88/2) sold under the name“Dow Corning 5225C Formulation Aid” by the company “Dow Corning.” (4)Oxyethylenated polydimethylsiloxane comprising a phosphate group, soldunder the name “Pecosil PS-100” by the company Phoenix Chemical. (5)Polyurethane powder sold under the name “Plastic Powder D-400” by thecompany

It was noted that the compositions of Examples 2 to 4 according to theinvention, after application to the skin, provide a satisfactorysoftness and do not feel tacky, whereas the composition of Example 1that is not part of the invention confers a tautness of the skin (nosoftness) and exhibits a tacky appearance.

The above written description of the invention provides a manner andprocess of making and using it such that any person skilled in this artis enabled to make and use the same, this enablement being provided inparticular for the subject matter of the appended claims, which make upa part of the original description and including a compositioncomprising, in a physiologically acceptable medium, at least onexanthine base or a plant extract containing it, at least onepolyurethane powder, and at least one non-ionic dimethicone copolyol.Also fully enabled is a cosmetic method for combating cellulite and/or“orange-peel” skin and/or slimming the figure, comprising the topicalapplication to the skin of a composition according to the invention. Inapreferred embodiment, the skin to which the composition is applied isskin showing signs of cellulite, or skin areas that commonly showcellulite with the aging process, etc.

As used above, the phrases “selected from the group consisting of,”“chosen from,” and the like include mixtures of the specified materials.

All references, patents, applications, tests, standards, documents,publications, brochures, texts, articles, etc. mentioned herein areincorporated herein by reference. Where a numerical limit or range isstated, the endpoints are included. Also, all values and subrangeswithin a numerical limit or range are specifically included as ifexplicitly written out. Terms such as “contain(s)” and the like as usedherein are open terms meaning ‘including at least’ unless otherwisespecifically noted.

The above description is presented to enable a person skilled in the artto make and use the invention, and is provided in the context of aparticular application and its requirements. Various modifications tothe preferred embodiments will be readily apparent to those skilled inthe art, and the generic principles defined herein may be applied toother embodiments and applications without departing from the spirit andscope of the invention. Thus, this invention is not intended to belimited to the embodiments shown, but is to be accorded the widest scopeconsistent with the principles and features disclosed herein.

The invention claimed is:
 1. A method for reducing tackiness associatedwith xanthine compound(s) in a composition containing at least onexanthine base, comprising adding at least one polyurethane powder and atleast one non-ionic dimethicone copolyol to the composition in an amountsufficient to reduce tackiness associated with the xanthine compound(s),wherein the xanthine base is present in the composition in an amountranging from 0.01% to 10% by weight, the polyurethane powder in anamount ranging from 0.5% to 10% by weight, and the non-ionic dimethiconecopolyol in an amount ranging from 0.05% to 5% by weight, all weightsbeing relative to the total weight of the composition.
 2. The methodaccording to claim 1, wherein the at least one xanthine base is selectedfrom the group consisting of caffeine, theophylline, theobromine,acefylline, xanthinol nicotinate, diniprophylline, diprophylline,etamiphylline, etophylline, proxyphylline, pentophylline,propentophylline, pyridophylline, bamiphylline, and mixtures thereof. 3.The method according to claim 1, wherein the at least one xanthine baseis selected from the group consisting of caffeine, theophylline,theobromine, acefylline, and mixtures thereof.
 4. The method accordingto claim 1, wherein the xanthine base is present in the composition inan amount ranging from 1% to 3% by weight, relative to the total weightof the composition.
 5. The method according to claim 1, wherein thepolyurethane powder is not film-forming.
 6. The method according toclaim 1, wherein the polyurethane powder is a powder of a copolymer ofhexamethylene diisocyanate and of trimethylol hexyl lactone.
 7. Themethod according to claim 1, wherein the composition comprises apolyurethane powder in an amount ranging from 0.5% to 3% by weightrelative to the weight of the total composition.
 8. The method accordingto claim 1, wherein the non-ionic dimethicone copolyol is anoxypropylenated and/or oxyethylenated polydimethylmethylsiloxane thatdoes not contain an ionic group.
 9. The method according to claim 1,wherein the non-ionic dimethicone copolyol is present in the compositionin an amount ranging from 0.1% to 2% by weight relative to the totalweight of the composition.
 10. The method according to claim 1, whereinthe composition further comprises an aqueous phase comprising water. 11.The method according to claim 10, wherein the composition compriseswater in an amount ranging from 30% to 80% by weight, relative to thetotal weight of the composition.
 12. The method according to claim 10,wherein the aqueous phase further comprises at least one monoalcoholhaving from 2 to 6 carbon atoms.
 13. The method according to claim 12,wherein the aqueous phase comprises at least one of ethanol andisopropanol.
 14. The method according to claim 12, wherein the at leastone monoalcohol is present in the composition in an amount ranging from1 to 30% by weight, relative to the total weight of the composition. 15.The method according to claim 1, wherein the composition comprises atleast one salicylic acid compound selected from the group consisting ofsalicylic acid, n-octanoyl salicylic acid, and mixtures thereof.
 16. Themethod according to claim 15, wherein the salicylic acid compound ispresent in the composition an amount ranging from 0.1% to 5% by weight,relative to the total weight of the composition.
 17. The methodaccording to claim 1, wherein the composition is in the form of anoil-in-water emulsion.
 18. The method according to claim 1, wherein thecomposition further comprises at least one active agent chosen fromactive agents that act on microcirculation, firming active agents,anti-glycant active agents, and mixtures thereof.
 19. The methodaccording to claim 1, wherein the composition comprises, relative to thetotal weight of the composition: 0.1% to 7% by weight of said at leastone xanthine base; 0.5% to 6% by weight of said at least onepolyurethane powder; and 0.1% to 3% by weight of said at least onenon-ionic dimethicone copolyol.
 20. The method according to claim 1,wherein the composition comprises, relative to the total weight of thecomposition: 1% to 3% by weight of said at least one xanthine base; 0.5%to 3% by weight of said at least one polyurethane powder; and 0.1% to 2%by weight of said at least one non-ionic dimethicone copolyol.